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1. 发明申请

WO2011100769A2 KINASE MODULATORS FOR THE TREATMENT OF CANCER 审中-公开
标题翻译：激酶调节剂治疗癌症
公开(公告)号：WO2011100769A2
公开(公告)日：2011-08-18
申请号：PCT/US2011/024947
申请日：2011-02-15
申请人： SYNOVO GMBH , BURNET, Michael , GUSE, Jan-Hinrich , BAUERLEIN, Christiane , HAHN, Ulrike
发明人： BURNET, Michael , GUSE, Jan-Hinrich , BAUERLEIN, Christiane , HAHN, Ulrike
IPC分类号： A61K31/4439 , A61K31/4427 , A61P35/00
CPC分类号： C07D231/38 , A61K31/415 , A61K31/4439 , A61K31/519 , A61K45/06 , A61K47/481 , A61K47/55 , C07D401/04 , C07D405/14 , C07D417/04 , C07D471/04 , C07H13/02 , A61K2300/00
摘要： A method of treating cancer in which a compound that inhibits the expression, production or release of IL-IO by immune cells is combined with a compound that stimulates the production of IL- 12 when given in combination with, or in the presence of TNFa. Said method is effective when provided in addition to standard therapies, notably chemotherapy using cytotoxic drugs and other forms of immune therapy including therapeutic vaccines.
摘要翻译：治疗癌症的方法，其中通过免疫细胞抑制IL-10的表达，产生或释放的化合物与当联合给予IL-12时刺激IL-12产生的化合物组合，或存在TNFα时。除了标准疗法之外，所述方法是有效的，特别是使用细胞毒性药物的化疗和其他形式的免疫疗法，包括治疗性疫苗。

2. 发明申请

WO2012051126A2 ANTI-INFLAMMATORY MACROLIDES 审中-公开
标题翻译：抗炎剂MACROLIDES
公开(公告)号：WO2012051126A2
公开(公告)日：2012-04-19
申请号：PCT/US2011/055657
申请日：2011-10-10
申请人： SYNOVO GMBH , BURNET, Michael , GUSE, Jan-Hinrich , BAEUERLEIN, Christiane , EGGERS, Mary
发明人： BURNET, Michael , GUSE, Jan-Hinrich , BAEUERLEIN, Christiane , EGGERS, Mary
IPC分类号： C07H17/08 , C07D413/12 , A61K31/7048 , A61P29/00
CPC分类号： C07H17/08
摘要： The invention provides novel compounds and compositions and methods for making and using the compounds and compositions.
摘要翻译：本发明提供了新型化合物和组合物以及制备和使用该化合物和组合物的方法。

3. 发明申请

WO2005027828A2 CONJUGATES OF BIOLOGICALLY ACTIVE COMPOUNDS, METHODS FOR THEIR PREPARATION AND USE, FORMULATION AND PHARMACEUTICAL APPLICATIONS THEREOF 审中-公开
标题翻译：生物活性化合物的偶联物，它们的制备和使用方法，制剂和药物应用
公开(公告)号：WO2005027828A2
公开(公告)日：2005-03-31
申请号：PCT/US2004/026485
申请日：2004-08-16
申请人： SYNOVO GMBH , GUTKE, Hans-Jurgen , FLOHR, Christian , BECK, Albert , MARGUTTI, Simona , EGGERS, Mary , GUSE, Jan-Hinrich , KHOBZAOUI, Moussa , BURNET, Michael
发明人： GUTKE, Hans-Jurgen , FLOHR, Christian , BECK, Albert , MARGUTTI, Simona , EGGERS, Mary , GUSE, Jan-Hinrich , KHOBZAOUI, Moussa , BURNET, Michael
IPC分类号： A61K
CPC分类号： C07H15/00 , A61K47/54 , A61K47/545 , A61K47/549 , A61K49/0004 , C07H17/08
摘要： This invention features a compound of the following formula: T-(-L-C) m , T is a transportophore, L is a bond or a linker having a molecular weight up to 240 dalton, C is a non-antibiotic therapeutic agent, and m is 1, 2, 3, 4, 5, 6, 7, or 8, in which the transportophore has an immune selectivity ratio of at least 2, the transportophore is covalently bonded to the non-antibiotic therapeutic agent via the bond or the linker, and the compound has an immune selectivity ratio of at least 2.
摘要翻译：本发明的特征在于具有下式的化合物：T - （ - LC）m，T是转运载体，L是键或连接基，其分子量高达至240道尔顿，C是非抗生素治疗剂，并且m是1,2,3,4,5,6,7或8，其中运输基团具有至少2的免疫选择性比率，运输基团是通过键或连接体与非抗生素治疗剂共价结合，并且该化合物具有至少2的免疫选择性比率。

4. 发明申请

WO2003070173A2 CONJUGATES OF BIOLOGICALLY ACTIVE COMPOUNDS, METHODS FOR THEIR PREPARATION AND USE, FORMULATION AND PHARMACEUTICAL APPLICATIONS THEREOF 审中-公开
标题翻译：生物活性化合物的偶联物，它们的制备和使用方法，制剂和药物应用
公开(公告)号：WO2003070173A2
公开(公告)日：2003-08-28
申请号：PCT/US2003/004596
申请日：2003-02-14
申请人： SYMPORE GMBH , BURNET, Michael , GUSE, Jan-Hinrich , KIM, Gene , BECK, Albert , TSOTSOU, Georgia , DROSTE-BOREL, Irina , BARKER, Laurence , WOLFF, Michael , GUTKE, Hans-Jurgen
发明人： BURNET, Michael , GUSE, Jan-Hinrich , KIM, Gene , BECK, Albert , TSOTSOU, Georgia , DROSTE-BOREL, Irina , BARKER, Laurence , WOLFF, Michael , GUTKE, Hans-Jurgen
IPC分类号： A61K
CPC分类号： B82Y5/00 , A61K47/552 , A61K47/556 , A61K47/67 , A61K49/0004 , G01N33/5047 , G01N33/5094
摘要： This invention features a method of identifying a compound useful for enhancing efficacy of a therapeutic agent. The method includes incubating a compound in blood cells; separating immune cells from erythrocytic cells; and determining the ratio of the concentration of the compound in the immune cells to the concentration of the compound in the erythrocytic cells; wherein the compound comprises a transportophore and a therapeutic agent, in which the transportophore is covalently bonded to the therapeutic agent via a bond or a linker.
摘要翻译：本发明的特征在于鉴定可用于增强治疗剂功效的化合物的方法。该方法包括在血细胞中孵育化合物; 从红细胞中分离免疫细胞; 并确定免疫细胞中化合物浓度与红细胞中化合物浓度的比率; 其中所述化合物包含转运载体和治疗剂，其中所述转运载体通过键或接头共价键合至治疗剂。

5. 发明申请

WO2003070254A1 ANTIBIOTIC CONJUGATES 审中-公开
标题翻译：抗生素联合
公开(公告)号：WO2003070254A1
公开(公告)日：2003-08-28
申请号：PCT/US2003/004714
申请日：2003-02-14
申请人： SYMPORE GMBH , BURNET, Michael , GUSE, Jan-Hinrich , KIM, Gene
发明人： BURNET, Michael , GUSE, Jan-Hinrich , KIM, Gene
IPC分类号： A61K31/70
CPC分类号： C07D273/00 , A61K31/7048 , A61K47/552 , C07D267/00 , C07D413/14 , C07D499/00 , C07H17/08
摘要： This invention features a compound of the following formula (I): wherein T is a transportophore, L is a bond or linker, and C is an antibiotic therapeutic agent, the transportophore is covalently bonded to the antibiotic therapeutic agent via the bond or the linker, and the transportophore is an azithromycin derivative or crown ether derivative.
摘要翻译：本发明的特征在于下列通式I的化合物：其中T是转运载体，L是一个键或连接体，C是一种抗生素治疗剂，该转运载体通过该键或连接体与抗生素治疗剂共价结合，以及转运蛋白是阿奇霉素衍生物或冠醚衍生物。

6. 发明申请

WO2003070174A2 CONJUGATES OF BIOLOGICALLY ACTIVE COMPOUNDS, METHODS FOR THEIR PREPARATION AND USE, FORMULATION AND PHARMACEUTICAL APPLICATIONS THEREOF 审中-公开
标题翻译：生物活性化合物的结合，其制备和使用方法，制剂和药物应用
公开(公告)号：WO2003070174A2
公开(公告)日：2003-08-28
申请号：PCT/US2003/004609
申请日：2003-02-14
申请人： SYMPORE GMBH , BURNET, Michael , GUSE, Jan-Hinrich , GUTKE, Hans-Jurgen , BECK, Albert , TSOTSOU, Georgia , DROSTE-BOREL, Irina , REICHERT, Jeannette , LUYTEN, Kattie , BUSCH, Maximilian , WOLFF, Michael , KHOBZAOUI, Moussa , MARGUTTI, Simona , MEINDL, Thomas , KIM, Gene , BARKER, Laurence
发明人： BURNET, Michael , GUSE, Jan-Hinrich , GUTKE, Hans-Jurgen , BECK, Albert , TSOTSOU, Georgia , DROSTE-BOREL, Irina , REICHERT, Jeannette , LUYTEN, Kattie , BUSCH, Maximilian , WOLFF, Michael , KHOBZAOUI, Moussa , MARGUTTI, Simona , MEINDL, Thomas , KIM, Gene , BARKER, Laurence
IPC分类号： A61K
CPC分类号： A61K49/0004 , A61K47/54 , A61K47/545 , A61K47/549
摘要： This invention features a compound of formula T-(-L-C) m, T is a transportophore, L is a bond or a linker having a molecular weight up to 240 dalton, C is a non-antibiotic therapeutic agent, and m is l, 2, 3, 4, 5, 6, 7, or 8, in which the transportophore has an immune selectivity ratio of at least 2, the transportophore is covalently bonded to the non-antibiotic therapeutic agent via the bond or the linker, and the compound has an immune selectivity ratio of at least 2.
摘要翻译：本发明的特征在于式T - （ - LC）m的化合物，T是转运载体，L是分子量高达240道尔顿的键或接头，C是非抗生素治疗剂，m是1， 2,3,4,5,6,7或8，其中转运载体具有至少2的免疫选择性比，转运载体通过键或连接体与非抗生素治疗剂共价结合，并且化合物的免疫选择性比至少为2。

7. 发明申请

WO2003070174A3 CONJUGATES OF BIOLOGICALLY ACTIVE COMPOUNDS, METHODS FOR THEIR PREPARATION AND USE, FORMULATION AND PHARMACEUTICAL APPLICATIONS THEREOF 审中-公开
公开(公告)号：WO2003070174A3
公开(公告)日：2003-08-28
申请号：PCT/US2003/004609
申请日：2003-02-14
申请人： SYMPORE GMBH , BURNET, Michael , GUSE, Jan-Hinrich , GUTKE, Hans-Jurgen , BECK, Albert , TSOTSOU, Georgia , DROSTE-BOREL, Irina , REICHERT, Jeannette , LUYTEN, Kattie , BUSCH, Maximilian , WOLFF, Michael , KHOBZAOUI, Moussa , MARGUTTI, Simona , MEINDL, Thomas , KIM, Gene , BARKER, Laurence
发明人： BURNET, Michael , GUSE, Jan-Hinrich , GUTKE, Hans-Jurgen , BECK, Albert , TSOTSOU, Georgia , DROSTE-BOREL, Irina , REICHERT, Jeannette , LUYTEN, Kattie , BUSCH, Maximilian , WOLFF, Michael , KHOBZAOUI, Moussa , MARGUTTI, Simona , MEINDL, Thomas , KIM, Gene , BARKER, Laurence
IPC分类号： C07G11/00
摘要： This invention features a compound of the following formula T-(-L-C) m, wherein T is a transportophore (a transport mediating molecule), L is a a non-antibiotic therapeutic agent, and m is l- 8, in which the transportophore has an immune selectivity ratio of at least 2, the transportophore is covalently bonded to the non-antibiotic therapeutic agent via the bond or the linker, and the compound has an immune selectivity ratio of at least 2. Figure 1 depicts comparison of selective uptake of diverse structure types into white blood cells from a complex blood mix.

8. 发明申请

WO2003038092A1 METHOD FOR IDENTIFYING TRANSPORT PROTEINS 审中-公开
标题翻译：识别运输蛋白的方法
公开(公告)号：WO2003038092A1
公开(公告)日：2003-05-08
申请号：PCT/AU2002/001480
申请日：2002-11-01
申请人： SYMPORE GMBH , KIM, Eugene, J. , BARKER, Laurence , BURNET, Michael , GUSE, Jan-Hinrich , LUYTEN, Kattie , TSOTSOU, Georgia
发明人： KIM, Eugene, J. , BARKER, Laurence , BURNET, Michael , GUSE, Jan-Hinrich , LUYTEN, Kattie , TSOTSOU, Georgia
IPC分类号： C12N15/11
CPC分类号： C07K14/415 , C07K14/40 , C12N15/1051
摘要： The present invention relates to methods for identifying proteins with transport activities and methods of screening for compounds that interact with the transport proteins. In one aspect, the present invention relates to a method for identifying a transport protein, the method comprising: (i) transforming yeast cells with a library of expression constructs, wherein one or more of the expression constructs comprises a polynucleotide encoding a putative transport protein; (ii) contacting the transformed yeast cells with a fluorescent substrate for the transport protein under conditions such that cells comprising an expression construct encoding a transport protein express the transport protein and thereby bind or internalise the fluorescent substrate; and (iii) isolating transformed yeast cells that exhibit uptake of the fluorescent substrate.
摘要翻译：本发明涉及用于鉴定具有转运活性的蛋白质的方法和筛选与转运蛋白相互作用的化合物的方法。一方面，本发明涉及用于鉴定转运蛋白的方法，所述方法包括：（i）用表达构建体文库转化酵母细胞，其中一个或多个表达构建体包含编码推定的转运蛋白的多核苷酸 ; （ii）使转化的酵母细胞与转运蛋白的荧光底物接触，条件是使包含编码转运蛋白的表达构建体的细胞表达转运蛋白，从而结合或内化荧光底物; 和（iii）分离表现出荧光底物摄取的转化的酵母细胞。

9. 发明申请

WO2011040956A1 NOVEL PESTICIDE FORMULATIONS 审中-公开
标题翻译：新型农药配方
公开(公告)号：WO2011040956A1
公开(公告)日：2011-04-07
申请号：PCT/US2010/002633
申请日：2010-09-29
申请人： BURNET, Michael , GUSE, Jan-Hinrich , REISSER, Martin
发明人： BURNET, Michael , GUSE, Jan-Hinrich , REISSER, Martin
IPC分类号： A61K9/14 , A01N25/26
CPC分类号： A01N25/10 , A01N37/34 , A01N37/40 , A01N39/04 , A01N41/10 , A01N43/50 , A01N43/54 , A01N43/653 , A01N43/70 , A01N47/36 , A01N47/40 , A01N51/00 , A01N57/20
摘要： Bioactive substances are imbedded or mixed into functionalized matrices to form homogenous water-insoluble solid complexes with desirable field properties such as reduced leaching in soil, improved leaf retention, selective unloading to roots and convenient packaging and application. Bioactive substances of this disclosure include pharmaceutical agents and pesticides including herbicides, insecticides, bacteriocides, rodenticides, nematicide and fungicides. The matrices comprise a monomeric-, oligomeric- or (co)polymeric backbone which may be derivatized with chemical groups exhibiting ionic (amines, carboxyls), hydrophobic, and ligandbinding interactions to form the matrix of the formulation. The various matrices may be mixed with additives or modifiers, grafted, or fused to obtain optimal properties. The formulations may be applied as granules, suspensions, emulsions in sprays, foams, or coats for seeds and fertilizers. Alternatively they may be melted and sprayed as concentrates. The formulations may be applied to foliage, soil, irrigation water, construction materials, seeding materials, grains, and buildings.
摘要翻译：将生物活性物质嵌入或混合到功能化基质中以形成具有期望的场性质的均匀的水不溶性固体复合物，例如在土壤中减少的浸出，改善的叶保留，对根的选择性卸载以及方便的包装和施用。本公开的生物活性物质包括药剂和农药，包括除草剂，杀虫剂，杀菌剂，杀鼠剂，杀线虫剂和杀真菌剂。该基质包括单体，低聚或（共）聚合物骨架，其可以用显示出离子（胺，羧基），疏水性和配体结合相互作用的化学基团衍生化以形成制剂的基质。可以将各种基质与添加剂或改性剂混合，接枝或熔融以获得最佳性能。制剂可以作为颗粒，悬浮液，喷雾剂，乳状液或用于种子和肥料的涂层的乳液施用。或者，它们可以被熔化并作为浓缩物喷雾。制剂可以应用于叶子，土壤，灌溉水，建筑材料，播种材料，谷物和建筑物。

10. 发明申请

WO2003070173A3 CONJUGATES OF BIOLOGICALLY ACTIVE COMPOUNDS, METHODS FOR THEIR PREPARATION AND USE, FORMULATION AND PHARMACEUTICAL APPLICATIONS THEREOF 审中-公开
公开(公告)号：WO2003070173A3
公开(公告)日：2003-08-28
申请号：PCT/US2003/004596
申请日：2003-02-14
申请人： SYMPORE GMBH , BURNET, Michael , GUSE, Jan-Hinrich , KIM, Gene , BECK, Albert , TSOTSOU, Georgia , DROSTE-BOREL, Irina , BARKER, Laurence , WOLFF, Michael , GUTKE, Hans-Jurgen
发明人： BURNET, Michael , GUSE, Jan-Hinrich , KIM, Gene , BECK, Albert , TSOTSOU, Georgia , DROSTE-BOREL, Irina , BARKER, Laurence , WOLFF, Michael , GUTKE, Hans-Jurgen
IPC分类号： G01N33/53
摘要： This invention features a method of identifying a compound useful for enhancing efficacy of a therapeutic agent. The method includes incubating a compound in blood cells; separating immune cells from erythrocytic cells; and determining the ratio of the concentration of the compound in the immune cells to the concentration of the compound in the erythrocytic cells; wherein the compound comprises a transportophore and a therapeutic agent, in which the transportophore is covalently bonded to the therapeutic agent via a bond or a linker.

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